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肽基-tRNA水解酶筛选结合分子对接揭示了琼氏蒲桃树皮提取物的抗生素潜力。

Peptidyl-tRNA hydrolase screening combined with molecular docking reveals the antibiotic potential of Syzygium johnsonii bark extract.

作者信息

Harris Sarah M, McFeeters Hana, Ogungbe Ifedayo V, Cruz-Vera Luis R, Setzer William N, Jackes Betsy R, McFeeters Robert L

机构信息

Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA.

出版信息

Nat Prod Commun. 2011 Oct;6(10):1421-4.

Abstract

With the rapid rise of antibiotic resistance in pathogenic bacteria, the need for new antibacterial agents is overwhelming. Herein we report the limited screening of tropical plant extracts for inhibitory activity against the essential enzyme peptidyl-tRNA hydrolase (Pth). Initial screening was conducted through an electrophoretic mobility assay and Northern blot detection. The ability of Pth to cleave the peptide-tRNA ester bond was assessed. The ethanol bark extract of Syzygium johnsonii showed strong inhibitory potential. Molecular docking studies point to Syzygium polyphenolics as the potential source of inhibition. This work is the forerunner of activity-directed isolation, purification, and structure elucidation of the inhibitory components from Syzygium johnsonii extracts and studies of compound interaction with Pth.

摘要

随着病原菌对抗生素耐药性的迅速上升,对新型抗菌剂的需求极为迫切。在此,我们报告了对热带植物提取物针对必需酶肽基 - tRNA水解酶(Pth)的抑制活性进行的有限筛选。初步筛选通过电泳迁移率测定和Northern印迹检测进行。评估了Pth切割肽 - tRNA酯键的能力。琼氏蒲桃的乙醇树皮提取物显示出很强的抑制潜力。分子对接研究表明琼氏蒲桃中的多酚类物质是潜在的抑制来源。这项工作是从琼氏蒲桃提取物中进行活性导向的抑制成分分离、纯化和结构解析以及化合物与Pth相互作用研究的先驱。

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